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Cancer Chemother Pharmacol. 2005 Sep;56(3):231-8. Epub 2005 Apr 19.

Is there a pharmacological basis for differences in 5-HT3-receptor antagonist efficacy in refractory patients?

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  • 1Rotterdam Cancer Institute, Groene Hilledijk 301, 3075, Rotterdam, The Netherlands.


5-HT3-receptor antagonists are the current antiemetic 'gold standard' for chemotherapy- and radiotherapy-induced nausea and vomiting. Interestingly, studies have shown that patients experiencing poor control of acute chemotherapy-induced nausea and vomiting with one antiemetic therapy may respond well to another agent, including a drug of the same class. This review examines pharmacological differences between the 5-HT3-receptor antagonists in order to determine potential reasons for their differing efficacy, particularly in relation to refractory emesis. Differences in drug metabolism by the cytochrome P450 system, inadequate dosing of the respective agents, differences in onset and duration of action, and effects on serotonin release and reuptake are discussed.

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